海洋链霉菌B170167发酵产物中含氮化合物及其细胞毒活性研究

利用色谱层析技术从海洋链霉菌B170167中分离得到11个含氮化合物,包括8个吲哚类和3个含氮杂环化合物。经波谱分析分别鉴定为Turbomycin A(1)、3,3-二-(3-吲哚)丙烷-1,2-二醇(2)、N-(2-(1H-Indol-3-yl)-2-oxoethyl)-acetamide(3)、N-乙酰基色氨酸(4)、9H-吡啶并[3,4-b]吲哚(5)、吲哚-3-甲醛(6)、3-吲哚丙酸(7)、3-吲哚甲酸(8)、光色素(9)、Ferrioxamine E(10)、3-羟基-2-甲基吡啶(11)。其中化合物11为首次从微生物中分离得到。化合物1、2、5、10、11显示出显著的细胞毒活性,化合物3、4、6、7、8显示中等程度的细胞毒活性。     

海洋链霉菌S09的化学成分研究(英文)

从海洋链霉菌S09的发酵液提取物中分离得到6个化合物,通过波谱技术分别鉴定为:thymidine(1)、尿嘧啶(2)、3-甲基-2,5-哌嗪二酮(3)、2-吡咯甲酸(4)、卡拉霉素(5)和β-咔啉(6)。海虾致死实验结果显示:化合物5在10μg/mL的浓度下对丰年虾的致死率为87.6%,显示出较强的细胞毒活性。     

中国南海海洋链霉菌Streptomyces sp.rssa1的化学成分研究

对中国南海珊瑚样品来源的链霉菌Streptomyces sp.rssa1代谢产物进行研究。采用正相硅胶柱、ODS反相硅胶柱、Sephadex LH-20凝胶柱以及半制备高效液相色谱等分离方法,从该菌株的大米固体培养基发酵产物中分离得到10个化合物,通过NMR、MS等波谱数据,将化合物结构分别鉴定为四霉素A(1)、四霉素B(2)、kanglemycin M(3)、tryptophandehydrobutyrine diketopiperazine(4)、3-吲哚乙酰胺(5)、N-乙酰基色氨酸(6)、苯乙酸(7)、N-乙酰基酪胺(8)、苯甲酰胺(9)、苯乙酰胺(10)。抗菌活性筛选显示,化合物4对溶藻弧菌(Vibrio alginolyticus)的生长具有弱抑制活性。细胞毒活性测试结果显示,化合物3对巨噬细胞RAW 264.7具有细胞毒活性。环化核苷酸磷酸二酯酶PDE4水解抑制活性筛选未发现化合物在测试浓度下具有抑制活性。     

链霉菌YIM69228发酵液中化学成分的研究

对链霉菌YIM69228发酵液进行了化学成分的研究,从中分离得到十个化合物。根据波谱数据分析,鉴定其结构分别为:(S)-2-羟基-3-(4-甲氧基苯基)-丙酸(1),异莨菪亭(2),N-苯乙基乙酰胺(3),肉桂酸(4),丁二酸单甲酯(5),3,4-二羟基苯甲酸(6),海藻糖(7),吐叶醇(8),Citroside A(9),苄基-β-D-吡喃木糖基-(1″-6’)-β-D-吡喃葡萄糖苷(10)。首次鉴定了天然产物化合物1的构型,其中化合物8～10为首次从链霉菌属放线菌中分离得到。     

相思子化学成分研究

本研究从相思子种子的乙醇提取物中首次分离得到8个化合物,通过理化性质及光谱分析鉴定其结构为N-9-甲基-β-咔啉(1)、异喹啉酮(2)、吲哚-3-羧酸(3)、2,3-二甲氧基-5,7-二羟基-二氢黄酮(4)、3-羟甲基呋喃醛(5)、3-羟基-2-甲基-4-吡喃酮(6)、豆甾醇-4,22-二烯-3-酮(7)和(6E,6’E)-2-hydroxypropane-1,3-diylbis(octadec-6-enoate)(8)。同时还得到13个其他成分。     

人参内生球毛壳菌株RSQMK-9的化学成分研究

从人参内生球毛壳菌株RSQMK-9的发酵培养物中提取分离得到14个代谢产物,通过波谱分析鉴定其结构分别为麦角甾醇(1)、4,6,8,22-四烯-3-酮-麦角甾烷(2)、啤酒甾醇(3)、9(11)-去氢麦角甾醇过氧化物(4)、alternariol(5)、大黄素甲醚(6)、3-吲哚甲酸(7)、2,3,4-三甲基-5,7-二羟基-2,3-二氢苯并呋喃(8)、2-氨基苯甲酰胺(9)、2-氨基苯甲酸(10)、3-甲基苔色酸(11)、甘露醇(12)、chaetoglobosin A(13)及5'-epichaetovirdin A(14)。这些化合物均为首次从人参内生球毛壳菌中发现,而且化合物6为首次从该属真菌中分离到。海虾致死试验结果显示:10μg/mL浓度下,化合物13和14对丰年虾的致死率分别为83.4%和54.3%。     

人参内生球毛壳菌株RSQMK-9的化学成分研究北大核心CSCD

从人参内生球毛壳菌株RSQMK-9的发酵培养物中提取分离得到14个代谢产物,通过波谱分析鉴定其结构分别为麦角甾醇(1)、4,6,8,22-四烯-3-酮-麦角甾烷(2)、啤酒甾醇(3)、9(11)-去氢麦角甾醇过氧化物(4)、alternariol(5)、大黄素甲醚(6)、3-吲哚甲酸(7)、2,3,4-三甲基-5,7-二羟基-2,3-二氢苯并呋喃(8)、2-氨基苯甲酰胺(9)、2-氨基苯甲酸(10)、3-甲基苔色酸(11)、甘露醇(12)、chaetoglobosin A(13)及5'-epichaetovirdin A(14)。这些化合物均为首次从人参内生球毛壳菌中发现,而且化合物6为首次从该属真菌中分离到。海虾致死试验结果显示:10μg/mL浓度下,化合物13和14对丰年虾的致死率分别为83.4%和54.3%。     

灰毛豆叶片的化学成分研究

从灰毛豆叶片中分离得到10个化合物,通过波谱数据和理化性质分别鉴定为:stigmast-1,5-dien-3β-ol(1),clemaphenol A(2),松脂醇(3),桉素(4),3-吲哚甲醛(5),色氨酸(6),(S)-4-苄基-2-噁唑烷酮(7),4-羟基苯基丙酸(8),buteaspermanol(9),bovatachalcone(10)。其中化合物1、2、4、5、7、8、9首次从该植物中分离得到。     

内生条纹拟盘多毛孢发酵液中细胞毒活性成分研究

从条纹拟盘多毛孢Pestalotopsis virgatula发酵液中分离得到8个化合物,其结构分别被鉴定为：2-(1-甲氧基-1-H-吲哚-3-基)乙醇 (1),2-(1-甲氧基-1-H-吲哚-3-基)乙酸 (2),3β-羟基-5α,8α-过氧化麦角甾-6,22-二烯 (3),麦角甾-4,6,8(14),22-四烯-3-酮 (4),对羟基苯乙醇 (5),邻苯二甲酸二异丁酯 (6),(E)-3-(4-羟基-3-甲氧苯基)败脂酸 (7) 和丁二酸 (8),化合物1–8均为首次从该菌种中分离得到。利用MTT法测试了化合物1 和2对5种人体肿瘤细胞的细胞毒活性,结果显示化合物1和2对5株肿瘤细胞株均具有一定选择性抑制活性。     

鸦胆子药渣的化学成分研究

为了解鸦胆子(Brucea javanica)药渣的化学成分,从中分离得到了10个化合物,经波谱分析分别鉴定为对羟基苯甲酸(1)、对羟基苯甲醛(2)、3,4-二羟基苯甲酸(3)、3,4-二羟基苯甲醛(4)、松柏醛(5)、芥子醛(6)、3-吲哚甲醛(7)、3-吲哚甲酸(8)、β-谷甾醇(9)和鸦胆苦醇(10)。其中化合物4～6、8为首次从鸦胆子分离得到。     

Xanthones from a microfungus of the genus Xylaria

Chemical investigations of a microfungus Xylaria sp. isolated from the Australian rainforest tree Glochidion ferdinandi have afforded two new natural products, 2-hydroxy-6-methyl-8-methoxy-9-oxo-9H-xanthene-1-carboxylic acid (1) and 2-hydroxy-6-hydroxymethyl-8-methoxy-9-oxo-9H-xanthene-1-carboxylic acid (2). Compound 1 has previously been synthesised but only partially characterised. Methylation of 1 using diazomethane afforded the crystalline compound 2,8-dimethoxy-6-methyl-9-oxo-9H-xanthene-1-carboxylic acid methyl ester (3), whose structure was determined by single crystal X-ray analysis. This paper reports the full spectroscopic characterisation of compounds 1-3 by NMR, UV, IR and MS data. All compounds were inactive in a brine shrimp lethality assay and several antimicrobial screens.     

霸王鞭乙酸乙酯部分化学成分研究

为了研究霸王鞭(Euphorbia royleana Boiss.)的化学成分及其卤虫致死活性,采用正相硅胶柱色谱、Sephadex LH-20凝胶柱色谱及半制备型高效液相色谱等方法从霸王鞭甲醇提取物的乙酸乙酯萃取部位中分离得到15个化合物。通过现代波谱学技术鉴定它们的结构分别为5(6)-guten-3α-ol(1)、蒲公英赛醇(2)、异蒲公英赛醇(3)、熊果酸(4)、齐墩果酸(5)、1-羟基-3,7,8-三甲氧基黄酮(6)、甲基獐牙菜素(7)、槲皮素(8)、胡萝卜苷(9)、β-谷甾醇(10)、豆甾醇(11)、香草醛(12)、十二烷醇(13)、植物醇(14)、1-[(12 E,16 E)-12,16-二十碳二烯酰基]-2-[(E,E)-7,11-十八碳二烯酰基]-3-硬脂酰基甘油(15)。化合物1、3、4、5、6、7、12、13、14和15均首次从该植物中分离得到。对所得到的化合物进行了卤虫致死活性研究,发现化合物4表现出较强卤虫致死活性,其LD₅₀为7.687μM。     

Lipid composition of three geographical sources of brine shrimp nauplii (Artemia sp.)

• 1.1. Percentage of triacylglycerols (TG), free fatty acids (FFA) and phospholipids (PL) in the total lipids, the fatty acid composition of each of these lipid classes, and the percentage of cholesterol were determined by gas chromatography in three geographical sources (San Francisco Bay, SFB; Chinese, CH; Colombian, COL) of brine shrim (Artemia sp.) nauplii.
• 2.2. There were no significant differences among sources of brine shrimp in total lipids, TG or FFA with means for all sources of 17.8, 65.8 and 10.9%, respectively. Percentage of phospholipid was significantly higher in SFB and CH sources of brine shrimp, 25.1 and 26.5%, respectively, than in COL 18.3%.
• 3.3. Marked differences in percentages of 18:3 (n-3) (linolenic acid) and 20:5 (n-3) (eicosapentaenoic acid or EPA) were found among brine shrimp sources, and concentration of these two fatty acids were usually inversely related within sources. The CH source contained higher concentrations of EPA ( > 9.0%) than the COL and SFB sources (< 5.0%) in all three lipid classes analyzed. No 22:6 (n-3) (docosahexaenoic acid or DHA) was found in any brine shrimp source.
• 4.4. Fatty acid compositions of the TG and PL were similar and did not differ among sources of brine shrimp, while the FFA had a lower percentage of polyunsaturated fatty acids, but was similar among sources of brine shrimp.
• 5.5. Differences in n-3 fatty acid composition indicated a difference in nutritional quality among sources of brine shrimp for feeding larval fish.

     

银杏内生菌Chaetomium globosum ZY-22次生代谢产物分离鉴定

采用柱层析方法从银杏叶内生真菌Chaetomium globosum ZY-22的培养菌丝体提取物中分离得到脑苷脂B(1)、脑苷脂C(2)、尿囊素(3)、9(11)-去氢麦角甾醇过氧化物(4)以及4,6,8,22-四烯-3-酮-麦角甾烷(5)和球毛壳甲素(6)共6个次生代谢物;经波谱分析确定了6个化合物的结构,其中脑苷脂B、脑苷脂C和尿囊素是首次从内生真菌中得到;海虾致死试验结果显示,化合物1～6在10 μg/mL浓度下对丰年虾的致死率分别为1.6%、4.2%、7.4%、16.9%、12.8%、83.6%、表明球毛壳甲素对海虾表现出很强的毒性作用.     

Labdane and pimarane diterpenes from Croton joufra

From the chloroform extract of the leaves of Croton joufra, the diterpenes 2alpha,3alpha-dihydroxy-labda-8(17),12(13),14(15)-triene and 3beta-hydroxy-19-O-acetyl-pimara-8(9),15-dien-7-one, were isolated. Their structures were established by spectroscopic methods. One of the compounds showed weak lethality in the brine shrimp assay.     

Energy Budgets for Eared Grebes on the Great Salt Lake and Implications for Harvest of Brine Shrimp

ABSTRACT About 1.5-million eared grebes (Podiceps nigricollis), representing half of the North American population, stage on Utah's Great Salt Lake, USA (GSL) during autumn migration to forage on brine shrimp (Artemia franciscana). Indirectly competing with birds for brine shrimp are commercial harvesters who annually collect >1 million kg (dry wt) of shrimp cysts (i.e., hardened eggs), an amount that during some years equals up to half of all brine shrimp cysts produced annually on the GSL. No information was available regarding what impact this commercial harvest was having on eared grebes. We determined daily energy requirements of eared grebes so that regulations governing brine shrimp cyst harvest would better reflect foraging needs of grebes. We measured basal metabolic rate (BMR) of eared grebes from June 2000 to October 2000. Mean BMR of 106 adult and subadult eared grebes was 0.023 kJ/g/hour (SD = 0.004), and mean BMR of 37 juveniles was 0.024 kJ/g/hour (SD = 0.003). Resting and preening metabolic rates were 1.2 times higher than BMR, whereas diving-bout metabolic rate was 1.7 times higher than BMR. Daily energy needs of an average-sized grebe (550 g) during November were 391 kJ. Meeting this energy need requires daily consumption of 24,400 adult brine shrimp. In addition, grebes must consume 2,100–5,200 adult shrimp daily to obtain enough energy reserves to continue their migration to California, USA, and Mexico. Hence, grebes need to consume 26,500–29,600 adult brine shrimp daily while staging on GSL. To achieve this high harvest rate, grebes need adult brine shrimp densities at >380 shrimp/m³during autumn. Commercial harvest of brine shrimp cysts from GSL should be curtailed when cyst densities fall below 20,000 cysts/m³to ensure enough adult brine shrimp for grebes during the subsequent year.     

Discovery and SAR of indole-2-carboxylic acid benzylidene-hydrazides as a new series of potent apoptosis inducers using a cell-based HTS assay

A series of indole-2-carboxylic acid benzylidene-hydrazides has been identified as a new class of potent apoptosis inducers through a novel cell-based caspase HTS assay. The screening hit, 5-chloro-3-methyl-indole-2-carboxylic acid (4-nitrobenzylidene)-hydrazide (3a), was found to arrest T47D cells in G(2)/M and to induce apoptosis as measured by the flow cytometric analysis assay. A SAR study was carried out by modification of the substitutions on the indole and benzene rings. Substitution at the 3-position of the indole ring was found to be important for apoptotic activity. A 20-fold increase of apoptotic activity was achieved from screening hit 3a to 5-methyl-3-phenyl-indole-2-carboxylic acid (4-methylbenzylidene)-hydrazide (9a) and 5-chloro-3-phenyl-indole-2-carboxylic acid (4-nitrobenzylidene)-hydrazide (9b), with EC(50) value of 0.1microM in the caspase activation assay in T47D breast cancer cells. Compound 9b also was found to be highly active in a standard growth inhibition assay with a GI(50) value of 0.9microM in T47D cells. Compound 3a and its analogs were found to inhibit tubulin polymerization, which is the most probable primary mechanism of action of these compounds.     

First synthesis of (+/-)-robinlin

The first synthesis of (+/-)-robinlin (1), a novel homo-monoterpene with strong bioactivity in the brine shrimp lethality test, was achieved by starting from 3-isobutyloxy-2,6,6-trimethyl-2-cyclohexen-1-one (2).     

Strobilols A-D: four cadinane-type sesquiterpenes from the edible mushroom Strobilurus ohshimae

Four sesquiterpenoids--strobilols A (1), B (2), C (3), and D (4)--were isolated from the organic extracts of fruiting bodies of the edible mushroom Strobilurus ohshimae. Their structures were determined by spectroscopic methods. Compound 1 exhibited moderate activity against the brine shrimp Artemia salina. This paper is the first report on isolation of cadinane-type sesquiterpenoids from S. ohshimae.     

刺山柑化学成分研究

采用硅胶、聚酰胺和Sephadex LH-20等色谱方法从维吾尔药刺山柑中分离得到11个化学成分,通过理化手段及波谱技术分别鉴定为正二十八烷(1)、β-胡萝卜苷(2)、正二十八烷醇(3)、正三十二烷酸(4)、正十六烷酸(5)、琥珀酸(6)、原儿茶酸(7)4、-羟基-5-甲基呋喃-3-羧酸(8)、山萘酚3-O-β-D-芸香糖苷(9)、芦丁(10)和水苏碱(11)。其中化合物13、和4为首次从该属植物中分离得到。